US4058612A
Expired / Lapsed
US
⏱️ 0.0 years remaining
6-(Polyhaloisopropyl)quinazoline-2,4-diones
Assignee: Merck Sharp & Dohme LLC
•
Filing: 1976-05-20
•
Granted: 1977-11-15
•
Expires: 1996-05-20
Abstract
Abstract Novel 6-(polyhaloisopropyl)quinazoline-2,4-diones, preparable from polyhaloisopropylarylureas, are disclosed herein. These compounds display potent hypotensive activity and are thus useful in the treatment of mammalian hypertension.
Inventors
- 👤 Bernard R. Neustadt
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 17:49
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/70; C07D239/72; C07D239/95; C07D239/96; C07C; C07C275/00; C07C275/28; C07C275/32; C07C275/34; C07C275/42; C07D263/00; C07D263/02; C07D263/08; C07D263/16; C07D263/28
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
68 words
A quinazoline-2,4-dione of the formula: ##STR4## wherein R 4 is a methyl, ethyl, 2-chloroethyl or 2-bromoethyl group; R 1 and R 3 are independently hydrogen, fluorine, chlorine, bromine, lower alkyl or lower alkoxy; Y, y 1 , y 2 and Y 3 are independently hydrogen, fluorine or chlorine; Z is hydrogen, chlorine, hydroxy or lower alkanoyloxy; and R is hydrogen, or alkyl having 1 to 4 carbon atoms.
Claim 2
Dependent Claim
68 words
A quinazoline-2,4-dione of the formula: ##STR4## wherein R 4 is a methyl, ethyl, 2-chloroethyl or 2-bromoethyl group; R 1 and R 3 are independently hydrogen, fluorine, chlorine, bromine, lower alkyl or lower alkoxy; Y, y 1 , y 2 and Y 3 are independently hydrogen, fluorine or chlorine; Z is hydrogen, chlorine, hydroxy or lower alkanoyloxy; and R is hydrogen, or alkyl having 1 to 4 carbon atoms.
Claim 3
Dependent Claim
12 words
A compound according to claim 1 wherein Z is a hydroxy group.
Claim 4
Dependent Claim
22 words
A compound according to claim 2 wherein Y, Y 1 , Y 2 and Y 3 are each independently fluorine or chlorine.
Claim 5
Dependent Claim
19 words
A compound according to claim 2 wherein Y, Y 1 , Y 2 and Y 3 are each fluorine.
Claim 6
Dependent Claim
15 words
A compound according to claim 2 wherein R, R 1 and R 3 are hydrogen.
Claim 7
Dependent Claim
9 words
A compound according to claim 3 which is 6-(chloro-2-hydroxypentafluoro-2-propyl)-3-ethyl-1-methylquinazoline-2,4-dione.
Claim 8
Dependent Claim
9 words
A compound according to claim 4 which is 3-ethyl-6-(hexafluoro-2-hydroxy-2-propyl)quinazoline-2,4-dione.
Claim 9
Dependent Claim
27 words
A pharmaceutical composition adopted to treat hypertension comprising an oral dosage of an antihypertensively effective amount of a compound of claim 1 in a pharmaceutically acceptable diluent.
Claim 10
Dependent Claim
15 words
A composition according to claim 8 in the form of a solid oral dosage unit.
Claim 11
Dependent Claim
11 words
A composition according to claim 8 wherein said compound is 3-ethyl-6-(hexafluoro-2-hydroxy-2-propyl)quinazoline-2,4-dione.
Claim 12
Dependent Claim
17 words
A method of treating hypertension comprising orally administering to a hypertensive mammal a composition of claim 8.
Claim 13
Dependent Claim
11 words
A method according to claim 11 wherein said composition comprises 3-ethyl-6-(hexafluoro-2-hydroxy-2-propyl)quinazoline-2,4-dione.
References Cited (Backward Citations)
US3794643A
Cited
US3879393A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-11-14 | 1981-05-16 | 1981-11-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-11-14 | 1985-05-16 | 1985-11-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-11-14 | 1989-05-16 | 1989-11-15 | $7700.00 | Window Closed / Lapsed |